Omidenepag isopropyl
Based on 1 Customer Validation
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering agent.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.17%
- CAS. Nr.: 1187451-19-9
- Formel: C26H28N6O4S
- Molecular Weight:520.60
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
HY-17642
OmidenepagEP2 Receptor Agonist -
HY-B0191
BimatoprostProstaglandin Analog -
HY-B0584
TravoprostFP Prostaglandin Receptor Agonist -
HY-B0600
TafluprostProstaglandin Receptor Agonist -
HY-108560
(+)-FluprostenolPTGER2 Agonist -
HY-B0584R
Travoprost (Standard) -
HY-B0600R
Tafluprost (Standard)Prostaglandin Receptor Agonist -
HY-108560R
(+)-Fluprostenol (Standard)PTGER2 Agonist
Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
EP2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4180 nM
Compound: OMDI
|
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
|
[PMID: 29995405] |
In Vivo
In ocular hypertensive monkeys finds that Omidenepag isopropyl lowers IOP by increasing both trabecular outflow facility and uveoscleral outflow[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 1187451-19-9
-
Appearance Solid
-
Molecular Weight 520.60
-
Formel C26H28N6O4S
-
Color White to off-white
-
SMILES
O=C(OC(C)C)CNC1=NC(CN(CC2=CC=C(N3N=CC=C3)C=C2)S(=O)(C4=CC=CN=C4)=O)=CC=C1
-
Synonyms
DE-117
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (96.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Kirihara T, et al. Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent. Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):145-153. [Content Brief]
[2]. Fuwa M, et al. Effects of a Novel Selective EP2 Receptor Agonist, Omidenepag Isopropyl, on Aqueous Humor Dynamics in Laser-Induced Ocular Hypertensive Monkeys. J Ocul Pharmacol Ther. 2018 Sep;34(7):531-537. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9209 mL | 9.6043 mL | 19.2086 mL | 48.0215 mL |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8417 mL | 9.6043 mL | |
| 10 mM | 0.1921 mL | 0.9604 mL | 1.9209 mL | 4.8022 mL | |
| 15 mM | 0.1281 mL | 0.6403 mL | 1.2806 mL | 3.2014 mL | |
| 20 mM | 0.0960 mL | 0.4802 mL | 0.9604 mL | 2.4011 mL | |
| 25 mM | 0.0768 mL | 0.3842 mL | 0.7683 mL | 1.9209 mL | |
| 30 mM | 0.0640 mL | 0.3201 mL | 0.6403 mL | 1.6007 mL | |
| 40 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2005 mL | |
| 50 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9604 mL | |
| 60 mM | 0.0320 mL | 0.1601 mL | 0.3201 mL | 0.8004 mL | |
| 80 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6003 mL |
Omidenepag isopropyl Related Classifications
HY-111406 Related Classifications
Powered by Bioz